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The aim of the research was to investigate the pharmacokinetics (PK) of enteric-coated mycophenolate sodium (EC-MPS) by quantification of the active metabolite of mycophenolic acid (MPA) after multiple escalating oral doses in Han kidney transplant recipients. A total of 28 Han postoperative kidney transplant recipients were given a multiple-dose of 540, 720 or 900 mg of EC-MPS two times a day in combination with tacrolimus for 6 days. Blood specimens were collected at each time point from 0 to 12 h after EC-MPS administration. MPA plasma concentrations were measured by UPLC-UV. The relationship between the EC-MPS dose and its PK parameters was assessed. In the range from 540 to 900 mg,and AUCdid not increase with dose escalation. The AUC,,andfor the 540 720 and 900 mg doses were not significantly different, respectively (>0.05). AUCandwere increased less than proportionally with increasing EC-MPS dose levels. Inter-individual variability in AUC,andwere considerable. Nonlinear PK relationships were found from the doses of 540-900 mg of EC-MPS.
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Objective To study compatibility stability of Danshen injection combined with dopamine injection in 5% glucose injection. Methods The relative contents of tanshinol sodium, protocatechuic aldehyde, rosmarinic acid,salvianolic acid B in Danshen injection and Dopamine hydrochloride in dopamine injection were determined by HPLC in 6h after the compatibility in the above infusion at 5 ℃,25℃,35 ℃ under dark and light,and the changes in pH value,appearance and insoluble particles were also observed.ResuIts There were no significant changes in appearance and pH value at 5℃,25℃,35 ℃ under dark,insoluble particles were in line with Chinese Pharmacopoeia,and the relative content of tanshinol sodium, protocatechuic aldehyde, rosmarinic acid,salvianolic acid B and Dopamine hydrochloride were above 99%(compared with 0h) in 6h.In the light conditions,as the temperature raised,the extension of storage time,the relative content of Dopamine hydrochloride was not significantly decreased,but the content of tanshinol sodium, protocatechuic aldehyde, rosmarinic acid and salvianolic acid B had declined,while pH value also had a certain degree of reduction,the insoluble particles had no obvious change.ConcIusion The mixture of Danshen injection and dopamine injection in 5%glucose injection is stable under dark conditions in 6h, illumination and temperature maybe the main factor affecting the stability of Danshen injection combined with dopamine injection.
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AIM:ToinvestigatetheeffectofIkarosisoformsontheproliferationofhumanovariancancerSK-OV3 cells.METHODS:Three isoforms of Ikaros, IK1, IK2 and IK6, were transfected into ovarian cancer SKOV3 cells. CCK-8 assay and cell counting were used to detect the effects of Ikaros isoforms on the proliferation of SKOV 3 cells.The cell cycle was analyzed by flow cytometry .The cell cycle-related proteins were detected by Western blot .RESULTS:IK1 and IK2 expression inhibited SKOV 3 cells proliferation .Flow cytometry analysis indicated that IK 1 and IK2 induced SK-OV3 cell cycle arrest at the G 1 phase.IK6 isoform exerted no obvious effect on the proliferation or cell cycle of SKOV 3 cells.Compared with control EV group , IK1 group and IK2 group showed a dramatic elevation in the expression of the cell cycle inhibitor p21, along with a substantial decrease in the expression of the cell cycle inducers cyclin D 1 and cyclin D2, which did not change in IK 6 group.CONCLUSION:IK1 and IK2 significantly inhibit the proliferation of ovarian cancer SKOV3 cells and induce cell cycle arrest at G 1 phase by regulation of cell cycle-related proteins cyclin D1, cyclin D2 and p21, while IK6 isoform exerts no obvious effect on the proliferation and cell cycle of SKOV 3 cells.
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Objective To evaluate the tissue compatibility of PLGA Nanoparticles and the effect of local intraluminal infusion of dexamethasone nanoparticles on restenosis after balloon angioplasty Methods PLGA nanoparticles were intraluminally administered after balloon injury in the rabbit iliac model Retention at different time points and biocompatibility of nanoparticles were evaluated Dexamethasone nanoparticles were also used in the same model to observe the effects on restenosis Results The PLGA nanoparticles apperaed to be fully biocompatible In the dexamethasone nanoparticles study, dexamethasone was presented in the treated segment for up to 14 days There is a significant reduction in intima/media ratio in treated animals compared with control Conclusion PLGA nanoparticles have good tissue compatibility Local administration of dexamethasone nanoparticles can retentate in vessel wall for more than 14 days and significantly decreased neointimal formation